Atypical Benzodiazepines Receptor Ligands

Who would think that a drug that most psychiatrists do not even consider to be a benzodiazepines can be more addictive than a benzodiazepines (benzos for short) drug? What exactly is Ambien (or Lunesta or a host of others for that matter) and why are they so addictive? Are they benzos or not and what is the big deal?

Officially there is a drug class called “Atypical Benzodiazepines Receptor Ligand” and most psychiatrists and doctors I talk to have no idea what that means. So let me spend a little time and explain since I have my pharmacology book handy; it will be easy to read but harder to reduce the complexity. I must also add that all doctors have learned what this is but it is so complicated they simply forget. As a result, doctors prescribe these drugs like candy yet they are worse than Valium, which is a real benzo. So what is the difference?

Let us start with the term “atypical” which will tell you that it is not a benzo but there is something about it that makes it fall into the benzo category. The term “benzodiazepines” represent a class of drugs that are known to be evil–they are not– and I will discuss that later. “Receptor” means a “hole” for lack of better word that sucks up the particular neurotransmitter that is able to fit into it. Think of a receptor like the kids’ toy of cubes and balls and other shapes fitting into the appropriate holes. It is very hard to fit a square object into a round hole. Thus the purpose of the specific receptors is to only accept the kind of neurotransmitters that fit that shape of receptor.

For regular benzos, this is exactly what is happening. They attach to the receptor they fit and behave there doing the job they do with the goal of dampening anxiety. Now let’s look at the most confusing of all terms “ligands.” Ligands do something very nasty. They reshape the receptor to make themselves fit, thereby modifying the neuron itself. This is very bad. Not only do they force themselves onto receptors they do not belong to, but they reshape the neuron to permit them to function as though they were benzos but they are not; they are hypnotics!

What does a hypnotics drug do? It places you into a trans of a completely unnatural state.It does not calm anxiety or reduce depression, it floats you into an outer existence for a while and then drops you back (crash) to reality.

There is also the little matter of “half-life” which causes a lot of problems.

Half life is the time it takes for the drug to have 50% of its active ingredients leave your body. Thus for Ambien it is 2.6 hours per wikipedia where you can find all benzos in their categories and dose equivalences as well. It is not listed how fast it completely leaves the system but one can calculate it pretty quick. Half leaves in 2.6 hours; half of the second half also leaves in 2.6 hours and so forth. When you add it all up, basically the drug is nearly undetectable in 15 hours but it is still in the body to a minuscule level. The problem is that it completely left in less than 24 hours. Most doctors think that having a benzo or alike with short half-life out of your system (less 24) hours is a good thing. I drew you a little chart here so you can see how bad that is.

Time to high and low

As you can see on my little hand drawn scribble here real benzos–particularly ones like Valium (orange)–have very long half-lives–some longer than a day. That means that if one is on Valium, for example, one never experiences highs and lows because before one can crash by having Valium leave the system, a new dose is taken at night and the cycle begins without any noticeable drop in level.

At the same time, if you look at what happens in the case of a receptor ligand (black), you can see that it peaks in about 1 hour and by 2.6 hours half the drug left the system. If the dose is chosen right for sleep, by the morning–8 hours after taking it–one is supposed to be without any trace of the hypnotics.

But we have a problem. The receptors were modified and want more of the stuff they used since now they have a weird shape and need to get more Ambien to fill up the receptor. Only another ligand can fill that receptor now.

Believe it or not, in as short a time as 3 days a person can get addicted to Ambien and experience withdrawals! The withdrawal itself comes with severe anxiety, lack of ability to sleep, sweating and being cold at the same time, shiver or shake uncontrollably, ready to run a Marathon but feeling totally ill. This is after 3 days of taking this drug.

So, if you are a doctor, a psychiatrist, a hospital nurse practitioner, a PA, anyone with the power to prescribe atypical benzodiazepines receptor ligands, think twice and do not!

There are more natural ways to get to sleep. It is way better to offer a turkey–serotonin—that puts people to sleep after lunch; it will do so after dinner as well–change light bulbs to pinkish/orange–blue light keeps people awake–take Vitamin A–this is my accidental discovery that A resets circadian rhythm in rats and apparently in me too. Maybe it will work for you as well. Take a walk if you can. Do not watch TV or be on the computer like I am now. Do not read–unless you have pink light and the paper of the book or magazine is not shiny to wake you up. Drink milk–a very good sleeping pill alternative for those who like it–I love it and drink a glass every evening before bed.

If you still cannot sleep, seek out sleep therapies, relaxation techniques and perhaps other, long acting benzos. Yes, they are addictive but no, they will not make you stupid as the current belief is. Do not take any serotonin medications since they are more addictive than benzos only doctors deny that… but I ask them to take one.. and then we’ll talk in the morning 2 days later.

Keep your health in your own control. There are way too many MDs out there who think your life is theirs to play with!Actually it is their lives that is in your hands since without you they do not get paid! Treat them like you would anyone else you pay for service, like a grocery clerk! If you don’t like the apple they give you, you complain! Right? At your MD it is not about an apple but your life and health so yes, do complain!

Your suggestions are welcome, as always!

Angela

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About Angela A Stanton, Ph.D.

Angela A Stanton, PhD, is a Neuroeconomist focusing on chronic pain--migraine in particular--, electrolyte homeostasis, nutrition, and genetics. She lives in Southern California. Her current research is focused on migraine cause, prevention and treatment without the use of medicines. As a forever migraineur from childhood, her discovery was helped by experimenting on herself. She found the cause of migraine to be at the ionic level, associated with disruption of the electrolyte homeostasis, resulting from genetic variations of all voltage gated channels that modulate electrolytes and voltage in the brain, insulin and glucose transporters, and several other related variants, such as the MTHFR variants of the B vitamin methylation process and many others. Migraineurs are glucose sensitive and should avoid eating carbs as much as possible.
She is working on the hypothesis that migraine is a metabolic disease.
As a result of the success of the first edition of her book and her research and findings after treating over 4000 migraineurs successfully world wide, all ages and both genders, she published the 2nd (extended) edition of her migraine book "Fighting The Migraine Epidemic: Complete Guide: How To Treat & Prevent Migraines Without Medications". The 2nd edition is the “holy grail” of migraine cause, development, treatment and prevention, incorporating all there is to know. It includes a long section with for medical and research professionals. The book is full of academic citations (over 800) to authenticate the statements she makes to be followed up by those interested and to spark further research interest. It is a "Complete Guide", published on September 29, 2017.
Dr. Stanton received her BSc at UCLA in Mathematics, MBA at UCR, MS in Management Science and Engineering at Stanford University, PhD in NeuroEconomics at Claremont Graduate University, and fMRI certification at Harvard University Medical School at the Martinos Center for Neuroimaging for experimenting with neurotransmitters on human volunteers, and is currently studying Functional Medicine. Dr. Stanton is an avid sports fan, currently enamored by resistance training and weight lifting, which she does three times a week with a private trainer. For relaxation (yeah.. about a half minute each day) Dr. Stanton paints and photographs. Follow her on Twitter at: @MigraineBook

14 Responses to 3 Days to Hell! Ambien!

I came across your site while doing some research on benzos and addiction. The Mayo Clinic website says Ambien is not as addictive as regular benzos – https://www.mayoclinic.org/diseases-conditions/insomnia/expert-answers/ambien/FAQ-20058103 – which is the opposite of what you say. Is this just another example of modern medicine being owned by the pharmaceutical industry or is there something else that might explain that? Also, if you have any recommendations for recent research on benzodiazepenes and aggression or violence please let me know. Thanks!

I suppose big pharma has a lot to do with what Mayo Clinic (or any other medical institutions) will say. The reasoning behind Ambien not being similarly addictive to otehr benzos is that it is an “atypical benodiazepine” because it really isn’t benzo only behaves like one. As a result, it is actually more addictive but causes different problems from taking, say, Valium. Valium (and other regular benzos) attach to the receptors properly, after all, they are “typical” meaning they connect the right way, with the right polarity, size, and shape. Atypical means that while they are not benzos, they connect to the same receptors to make the receptor believe that they grabbed onto benzos but then the actual chemical events that follow are different. This has two manifestations:

1) putting a square plug into a round hole can indeed be forced because protein structures (receptors) are flexible and the folds can be changed–and here is the second part
2) the folds have changed. In protein structure, the most important thing is how they are folded–that sets their function and purpose.

In the case of Ambien, the folds change and depending on the age of the person and his/her brain cell regeneration capability (requires the ketogenic diet with major fasting), the brain may or may not recover. It is this fold difference that makes Ambien into a hallucinogenic hypnotic drug as opposed to typical benzos, which work on the dopamine pathway to reduce and block anxiety. Two very different functions then and as a result, the addiction is also different. Whereas true benzos become “adaptive” (if prescribed properly) and not addictive–addictive means the need for seeking for more and more drug over time and the receptors get downregulated from over stimulation–and are hard to quit, Ambient becomes addictive because it not only downregulates the receptors but destroys them.

This is why Ambien is much worse for you to take than Valium or similar. The problem with benzos is that they are misprescribed. A benzo, such as Valium or Klonopin, has between 26 and 50 hours of hal-life, so taking one pill every other day is more than sufficient. Prescribing them 2-3 times a day (as MANY doctors do) make then addictive because the dose increases by 10-fold when a new pill is taken way before the drug has even reached its full power (Valium can take up to 4 hours to activate and if one takes it 3 times a day, that is a triple dose per day and in 3 days, when the first pill just reached half-life, the 10th pill is being taken! This is a tremendous mismanagement of prescriptions and which destroyed the reputation of otherwise completely safe and great medicines. There is nothing about them that would cause suicides if they are prescribed correctly. The problems is that they are not prescribed right.

Then there are the short-acting benzo nightmares, such as Ativan. Ativan has a very fast “high” and a short half-life (5-10 hours age, gender dependent) and as a result it has an extreme violent crash. The kind of drug that makes people jump out the window. This drug needs to be prescribed 3 times a day and it becomes addictive very fast.

So while there is no new science hitting the news and I have not been following research on this much, I can suggest that taking the right benzo with the right doctor who knows how to prescribe them is totally safe.

SAFETY WARNING: Benzodiazepines are strong anticholinergics, which are implicated in dangerously increasing one’s risk of dementia. All anticholinergic meds, whether prescribed or over the counter -— such as diphenhydramine (allergy meds and sleep aids) — should be avoided or taken for the shortest time and the smallest dose possible. Some of this memory-robbing side effect may not be reversible. Please check out the New York Times articles, as well as other news and medical websites.

Nora, the statement that benzodiazepines increase one’s risk of dementia is about 30 years old and is not true… The new drugs, be it SSRI or Topamax, or Lyrica or alike, however, create major memory problems immediately. And most are permanent even after 2 weeks of use. Stopping any of those medications takes years and now they also prescribe them to children. By contrast, I know several people who have been on benzos since early age before 20 and now in the 60’s are completely dementia free after 40 years of taking them. This dementia is a myth similarly to how salt is bad for you. A myth that was never proven only guessed.

I was addicted to Ambien for several years. It cause me to sleepwalk and sleep talk. I actually called friends at odd hours having weird conversations. My girlfriends mother at one point had considered calling 911! I would order all types of products online and then wonder why I was getting all these packages because I had no memory of what I had done. The only thing that didn’t suffer was my writing. In fact I wrote some very good poems while asleep. Later when I researched Ambien on WebMD and some other medical and health sites I found it Ambien was normally prescribe to people suffering from catatonia or catatonic stupor. Something like in the movie Awakenings when the lead character played by the late Robin Williams finds that L-dopa “awakens” hospital patients in a catatonic state. However if that is not your problem Ambien will cause you to sleep but the part of your brain that allows you to perform everyday functions is still awake so you do things you’d normally do plus some stuff you should not do. November 2012 I moved from Queens, NY to Brooklyn, NY. I finally stopped taking Ambien winter 2013 when I ran through my Brooklyn neighborhood in my nightclothes. Being that my neighborhood can be a little dicey this is a very dangerous thing for a woman to do. That was my wake-up call. Yes I still have insomnia which I chalk up to menopause but I make the most of being a Midnight Marauder by getting lots of writing done and my writing is much better without Ambien!

Wow Dancingpalmtree! This is an amazing story! I am glad you stopped taking it. I am not sure how long it takes for the receptors to return to normal since I have never taken the drug–and of course no book ever mentions THAT! I am glad you are off of it. I would love to read some of your poems; are they online?

As for helping you to sleep, consider those things I mentioned toward the end of the post. Those really do work. The Vitamin A find was completely coincidental (I will be calling that serendipity from now on). Take max 10,000IU a day with a fatty meal (fat soluble) unless you eat a lot of foods that contain A, such as carrots and liver. It will help.

How long did you take Ambien for and how long has it been that you stopped it? This will help me judge what happens to the shape of the receptor and how fast it can return to normal–if it can return to normal. I wish you well!!!

Let’s see I was erroneously diagnosed with a variety of mental problems in 1999. My mother had died in 1998 and what I really needed was grief counseling instead of being given a candy store of anti-depressants. I graduated from college in 2002 so I would guess the psychiatrist or what she really was a Legalized Pusher/Drug Dealer started giving me Ambien around 2003 or 2004. I was laid off from my job in 2006 and lost my medical insurance in 2007. Got a new job in 2008 and went back on Ambien mid to late 2008.

I have found when I was going to the gym on a regular basis earlier this year my sleep pattern improved. I stopped going because I injured my knee but hope to begin my workouts again very soon. I will try the Vitamin A capsules as I hate carrots and am trying to stay away from red meat.

Sorry to hear the struggle you had to go through! My mom died this year and I am battling the medical system because they killed her–luckily they did not kill you! I hope you will heal fast and can return to the gym. Exercise is the key to success no matter what way we look at it because it uses up all the stress hormones we release during the day. It is fantastic against anxiety–albeit for many it is not a cure but it definitely helps. Since you have no anxiety, you may find full benefit and recovery from the exercise. I followed your blog and will start reading. 🙂 Glad we connected!

Thanks Moongazer. I no longer have migraines since I wrote the book on how to prevent and get rid of migraines. 🙂 I got rid of mine 4 years ago when I figured out the cause and had none since–well I had 1 when I was out of the country and had no options to get what I needed. Getting rid of migraines is really simple. It is based on ionic balancing. I wrote a whole series of blogs on it and a book. Since you are in the UK the amazon UK link for e-book and for paperback. And the articles I wrote that may help you with migraines–start with the bottom article first.